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Improved quenched fluorescent probe for imaging of cysteine cathepsin activity.

Abstract
The cysteine cathepsins are a family of proteases that play important roles in both normal cellular physiology and many human diseases. In cancer, the activity of many of the cysteine cathepsins is upregulated and can be exploited for tumor imaging. Here we present the design and synthesis of a new class of quenched fluorescent activity-based probes (qABPs) containing a phenoxymethyl ketone (PMK) electrophile. These reagents show enhanced in vivo properties and broad reactivity resulting in dramatically improved labeling and tumor imaging properties compared to those of previously reported ABPs.
AuthorsMartijn Verdoes, Kristina Oresic Bender, Ehud Segal, Wouter A van der Linden, Salahuddin Syed, Nimali P Withana, Laura E Sanman, Matthew Bogyo
JournalJournal of the American Chemical Society (J Am Chem Soc) Vol. 135 Issue 39 Pg. 14726-30 (Oct 02 2013) ISSN: 1520-5126 [Electronic] United States
PMID23971698 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References
  • Fluorescent Dyes
  • Ketones
  • Cysteine Proteases
  • Cysteine
Topics
  • Animals
  • Breast (enzymology, pathology)
  • Breast Neoplasms (diagnosis, enzymology, pathology)
  • Cell Line
  • Cells, Cultured
  • Cysteine (metabolism)
  • Cysteine Proteases (analysis, metabolism)
  • Female
  • Fluorescent Dyes (chemical synthesis, chemistry)
  • Humans
  • Ketones (chemical synthesis, chemistry)
  • Mice
  • Optical Imaging (methods)

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